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. 2017 Jun 1;27(11):2439-2442.
doi: 10.1016/j.bmcl.2017.04.005. Epub 2017 Apr 4.

Pharmacological evaluation of a novel series of urea, thiourea and guanidine derivatives as P2X7 receptor antagonists

Erick C N Wong  1 , Tristan A Reekie  2 , Eryn L Werry  3 , James O'Brien-Brown  2 , Sarah L Bowyer  2 , Michael Kassiou  4
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Pharmacological evaluation of a novel series of urea, thiourea and guanidine derivatives as P2X7 receptor antagonists

Erick C N Wong et al. Bioorg Med Chem Lett. .

Abstract

We report on P2X7 receptor antagonists based on a lead adamantly-cyanoguanidine-aryl moiety. We have investigated the importance of the central cyanoguanidine moiety by replacing it with urea, thiourea or guanidine moieties. We have also investigated the linker length between the central moiety and the aryl portion. All compounds were assessed for their inhibitory potency in a pore-formation dye uptake assay at the P2X7 receptor. None of the compounds resulted in an improved potency illustrating the importance of the cyanoguanidine moiety in this chemotype.

Keywords: Cyanoguanidine; Inflammation; P2X(7)R; Thiourea; Urea.

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